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AR122069A2 - HETEROCYCLIC INHIBITORS OF BRUTON'S TYROSINE KINASE - Google Patents

HETEROCYCLIC INHIBITORS OF BRUTON'S TYROSINE KINASE

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Publication number
AR122069A2
AR122069A2 ARP210101299A ARP210101299A AR122069A2 AR 122069 A2 AR122069 A2 AR 122069A2 AR P210101299 A ARP210101299 A AR P210101299A AR P210101299 A ARP210101299 A AR P210101299A AR 122069 A2 AR122069 A2 AR 122069A2
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AR
Argentina
Prior art keywords
membered
ring
oxygen
nitrogen
sulfur
Prior art date
Application number
ARP210101299A
Other languages
Spanish (es)
Inventor
Brian T Hopkins
Tracy J Jenkins
Noel Powell
Laura Silvian
Deping Wang
Patrick Conlon
Julio H Cuervo
Bing Guan
Gnanasambandam Kumaravel
Alexey A Lugovskoy
Doug Marcotte
Daniel Scott
Art Teveras
Daniel A Erlanson
Min Zhong
Minna Bui
Junfa Fan
Original Assignee
Sunesis Pharmaceuticals Inc
Biogen Ma Inc
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Publication date
Application filed by Sunesis Pharmaceuticals Inc, Biogen Ma Inc filed Critical Sunesis Pharmaceuticals Inc
Publication of AR122069A2 publication Critical patent/AR122069A2/en

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    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

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  • Orthopedic Medicine & Surgery (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto que tiene la fórmula (1) en donde: X¹ es -O-, -CR⁵R⁶- o -NR⁷-; X² es =CR⁸- o =N-; p es 0 - 5; y es 0, 1, ó 2; z es 0, 1, ó 2, en donde z es 0 ó 1 cuando y es 2, y z es 1 ó 2 cuando y es 0; cada R¹ es independientemente halógeno, -NO₂, -CN, -OR, -SR, -N(R)₂, -C(O)R, -CO₂R, -C(O)C(O)R, -C(O)CH₂C(O)R, -S(O)R, -S(O)₂R, -C(O)N(R)₂, -SO₂N(R)₂, -OC(O)R, -N(R)C(O)R, -N(R)N(R)₂, -N(R)C(=NR)N(R)₂, -C(=NR)N(R)₂, -C=NOR, -N(R)C(O)N(R)₂, -N(R)SO₂N(R)₂, -N(R)SO₂R, -OC(O)N(R)₂, o un grupo opcionalmente sustituido seleccionado de alifático de C₁₋₁₂, fenilo, un anillo carbocíclico monocíclico insaturado parcialmente o saturado de 3 - 7 miembros, un anillo carbocíclico bicíclico insaturado parcialmente o saturado de 7 - 10 miembros, un anillo heterocíclico monocíclico insaturado parcialmente o saturado de 3 - 7 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, un anillo heterocíclico bicíclico insaturado parcialmente o saturado de 7 - 10 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, un anillo arilo bicíclico de 8 - 10 miembros, un anillo heteroarilo de 5 - 6 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, o un anillo heteroarilo bicíclico de 8 - 10 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno o azufre, o: dos grupos R¹ en átomos de carbono adyacentes juntos con sus átomos intermedios para formar un anillo sustituido opcionalmente de fenilo, un anillo carbocíclico monocíclico saturado o insaturado parcialmente de 3 - 7 miembros, un anillo carbocíclico bicíclico saturado o insaturado parcialmente de 7 - 10 miembros, un anillo heterocíclico monocíclico saturado o insaturado parcialmente de 3 - 7 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, un anillo heterocíclico bicíclico insaturado parcialmente o saturado de 7 - 10 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, un anillo arilo bicíclico de 8 - 10 miembros, un anillo heteroarilo de 5 - 6 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, o un anillo heteroarilo bicíclico de 8 - 10 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno o azufre, o: dos grupos R¹ en átomos de carbono no adyacentes se toman juntos con sus átomos intermedios para formar un puente opcionalmente sustituido de un grupo bicíclico con puente, en donde el puente es una cadena de hidrocarburo de C₁₋₃ en donde una unidad de metileno se reemplaza opcionalmente por -NR-, -O-, -C(O)-, -OC(O)-, -C(O)O-, -S-S-, o -S-, o: dos grupos R¹ en el mismo átomo de carbono se toman junto con sus átomos intermedios para formar un anillo espiro fusionado sustituido opcionalmente seleccionado de un anillo carbocíclico saturado o insaturado parcialmente de 3 - 7 miembros, o un anillo heterocíclico monocíclico saturado o insaturado parcialmente de 3 - 7 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre; cada R es independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático de C₁₋₆, fenilo, un anillo carbocíclico insaturado parcialmente o saturado de 3 - 7 miembros, un anillo heterocíclico monocíclico insaturado parcialmente o saturado de 3 - 7 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, o un anillo heteroarilo bicíclico de 5 - 6 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno o azufre, o: dos grupos R en el mismo nitrógeno se toman junto con sus átomos intermedios para formar un anillo saturado, parcialmente insaturado o heteroarilo de 3 - 7 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre; cada uno de R², R³, R⁵, R⁶, y R⁸ es independientemente R, halógeno, -NO₂, -CN, -OR, -SR, -N(R)₂, -C(O)R, -CO₂R, -C(O)C(O)R, -C(O)CH₂C(O)R, -S(O)R, -S(O)₂R, -C(O)N(R)₂, -SO₂N(R)₂, -OC(O)R, -N(R)C(O)R, -N(R)N(R)₂, -N(R)C(=NR)N(R)₂, -C(=NR)N(R)₂, -C=NOR, -N(R)C(O)N(R)₂, -N(R)SO₂N(R)₂, -N(R)SO₂R, o -OC(O)N(R)₂; o: R³ y R⁴ se toman opcionalmente junto con sus átomos intermedios para formar un anillo sustituido opcionalmente de un anillo heterocíclico monocíclico saturado o insaturado parcialmente de 3 - 7 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, o un anillo heterocíclico bicíclico insaturado parcialmente o saturado de 7 - 10 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre; cada uno de R⁴ y R⁷ es independientemente R, -CN, -C(O)R, -CO₂R, -C(O)C(O)R, -C(O)CH₂C(O)R, -C(O)N(R)₂, -S(O)R, -S(O)₂R, o -S(O)₂N(R)₂; El anillo A¹ es un anillo bivalente opcionalmente sustituido seleccionado de fenileno, un carbociclileno saturado o insaturado parcialmente de 3 - 8 miembros, un carbociclileno bicíclico saturado o insaturado parcialmente de 7 - 10 miembros, un heterociclileno monocíclico saturado o insaturado parcialmente de 3 - 8 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, un heterociclileno bicíclico insaturado parcialmente o saturado de 7 - 10 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, un arileno bicíclico de 8 - 10 miembros, un heteroarileno de 5 - 6 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, o un anillo heteroarileno bicíclico de 8 - 10 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno o azufre; Anillo A² es un anillo opcionalmente sustituido seleccionado de fenilo, un anillo carbocíclico monocíclico saturado o insaturado parcialmente de 3 - 7 miembros, un anillo carbocíclico bicíclico saturado o insaturado parcialmente de 7 - 10 miembros, un anillo heterocíclico monocíclico saturado o insaturado parcialmente de 3 - 7 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, un anillo heterocíclico bicíclico insaturado parcialmente o saturado de 7 - 10 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, un anillo arilo bicíclico de 8 - 10 miembros, un anillo heteroarilo de 5 - 6 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, o un anillo heteroarilo bicíclico de 8 - 10 miembros que tiene 1 - 4 heteroátomos seleccionados independientemente de nitrógeno, oxígeno o azufre; L es un enlace covalente o una cadena de hidrocarburo, recta o ramificada, saturada o insaturada, bivalente de C₁₋₇, opcionalmente sustituida, en donde uno, dos, o tres unidades metileno de L se reemplazan independientemente por -Cy-, -CR₂-, -NR-, -N(R)C(O)-, -C(O)N(R)-, -N(R)SO₂-, -SO₂N(R)-, -O-, -C(O)-, -OC(O)-, -C(O)O-, -S-, -SO-, -SO₂-, -C(=S)-, -C(=NR)-, -N=N-, o -C(=N₂)-, en donde al menos una unidad metileno de L se reemplaza por -N(R)-, y cada Cy es independientemente un anillo bivalente opcionalmente sustituido seleccionado de fenileno, un carbociclileno saturado o insaturado parcialmente de 3 - 7 miembros, un heterociclileno monocíclico saturado o insaturado parcialmente de 3 - 7 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente de nitrógeno, oxígeno, o azufre, o un heteroarileno de 5 - 6 miembros que tiene 1 - 3 heteroátomos seleccionados independientemente de oxígeno.Claim 1: A compound having the formula (1) wherein: X¹ is -O-, -CR⁵R⁶- or -NR⁷-; X² is =CR⁸- or =N-; p is 0-5; y is 0, 1, or 2; z is 0, 1, or 2, where z is 0 or 1 when y is 2, and z is 1 or 2 when y is 0; each R¹ is independently halogen, -NO₂, -CN, -OR, -SR, -N(R)₂, -C(O)R, -CO₂R, -C(O)C(O)R, -C(O )CH₂C(O)R, -S(O)R, -S(O)₂R, -C(O)N(R)₂, -SO₂N(R)₂, -OC(O)R, -N(R )C(O)R, -N(R)N(R)₂, -N(R)C(=NR)N(R)₂, -C(=NR)N(R)₂, -C=NOR , -N(R)C(O)N(R)₂, -N(R)SO₂N(R)₂, -N(R)SO₂R, -OC(O)N(R)₂, or an optionally substituted group selected from C₁₋₁₂ aliphatic, phenyl, a 3-7 membered saturated or partially unsaturated monocyclic carbocyclic ring, a 7-10 membered saturated or partially unsaturated bicyclic carbocyclic ring, a 3-7 membered saturated or partially unsaturated monocyclic heterocyclic ring members having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a 7-10 membered partially unsaturated or saturated bicyclic heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a bicyclic aryl ring 8-10 membered, a 5-6 membered heteroaryl ring having 1 - 3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-10 membered bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or: two R¹ groups on adjacent carbon atoms together with its intermediate atoms to form an optionally substituted phenyl ring, a 3-7 membered saturated or partially unsaturated monocyclic carbocyclic ring, a 7-10 membered saturated or partially unsaturated bicyclic carbocyclic ring, a 3-membered saturated or partially unsaturated monocyclic heterocyclic ring - 7 membered having 1 - 2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a 7 - 10 membered partially unsaturated or saturated bicyclic heterocyclic ring having 1 - 3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a ring 8-10 membered bicyclic aryl, a 5-6 membered heteroaryl ring s having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-10 membered bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or: two R¹ groups on non-adjacent carbons are taken together with their intervening atoms to form an optionally substituted bridge of a bridged bicyclic group, wherein the bridge is a C₁₋₃ hydrocarbon chain in which a methylene unit is optionally replaced by -NR-, -O-, -C(O)-, -OC(O)-, -C(O)O-, -S-S-, or -S-, or: two R¹ groups on the same carbon atom are taken together with its intermediate atoms to form a substituted fused spiro ring optionally selected from a 3-7 membered saturated or partially unsaturated carbocyclic ring, or a 3-7 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen o, oxygen, o sulfur; each R is independently hydrogen or an optionally substituted group selected from C₁₋₆ aliphatic, phenyl, a 3-7 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1- 2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered bicyclic heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or: two R groups on the same nitrogen are taken together with intermediate atoms thereof to form a 3-7 membered saturated, partially unsaturated, or heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of R², R³, R⁵, R⁶, and R⁸ is independently R, halogen, -NO₂, -CN, -OR, -SR, -N(R)₂, -C(O)R, -CO₂R, -C (O)C(O)R, -C(O)CH₂C(O)R, -S(O)R, -S(O)₂R, -C(O)N(R)₂, -SO₂N(R) ₂, -OC(O)R, -N(R)C(O)R, -N(R)N(R)₂, -N(R)C(=NR)N(R)₂, -C( =NR)N(R)₂, -C=NOR, -N(R)C(O)N(R)₂, -N(R)SO₂N(R)₂, -N(R)SO₂R, or -OC (O)N(R)₂; or: R³ and R⁴ are optionally taken together with their intermediate atoms to form an optionally substituted ring of a 3-7 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 7-10 membered saturated or partially unsaturated bicyclic heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of R⁴ and R⁷ is independently R, -CN, -C(O)R, -CO₂R, -C(O)C(O)R, -C(O)CH₂C(O)R, -C(O) N(R)₂, -S(O)R, -S(O)₂R, or -S(O)₂N(R)₂; Ring A¹ is an optionally substituted bivalent ring selected from phenylene, a 3-8 membered saturated or partially unsaturated carbocyclylene, a 7-10 membered saturated or partially unsaturated bicyclic carbocyclylene, a 3-8 membered saturated or partially unsaturated monocyclic heterocyclylene having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a 7-10 membered saturated or partially unsaturated bicyclic heterocyclylene having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, an 8- 10 membered, a 5-6 membered heteroarylene having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-10 membered bicyclic heteroarylene ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur ; Ring A² is an optionally substituted ring selected from phenyl, a 3-7 membered monocyclic saturated or partially unsaturated carbocyclic ring, a 7-10 membered bicyclic saturated or partially unsaturated carbocyclic ring, a 3-membered saturated or partially unsaturated monocyclic heterocyclic ring, 7-membered having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a partially unsaturated or saturated bicyclic heterocyclic ring 7-10-membered having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, an aryl ring 8-10 membered bicyclic, a 5-6 membered heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-10 membered bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen or sulfur; L is a covalent bond or an optionally substituted, straight or branched, saturated or unsaturated, bivalent C₁₋₇ hydrocarbon chain, wherein one, two, or three methylene units of L are independently replaced by -Cy-, -CR₂ -, -NR-, -N(R)C(O)-, -C(O)N(R)-, -N(R)SO₂-, -SO₂N(R)-, -O-, -C( O)-, -OC(O)-, -C(O)O-, -S-, -SO-, -SO₂-, -C(=S)-, -C(=NR)-, -N= N-, or -C(=N₂)-, wherein at least one methylene unit of L is replaced by -N(R)-, and each Cy is independently an optionally substituted bivalent ring selected from phenylene, a saturated or unsaturated carbocyclylene partially 3-7 membered, a 3-7 membered partially saturated or unsaturated monocyclic heterocyclylene having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered heteroarylene having 1-3 heteroatoms selected regardless of oxygen.

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Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011029043A1 (en) 2009-09-04 2011-03-10 Biogen Idec Ma Inc. Heteroaryl btk inhibitors
DK2473049T3 (en) * 2009-09-04 2019-04-01 Biogen Ma Inc INHIBITORS OF BRUTON'S TYROSINKINASE
BR112012029395A2 (en) * 2010-05-17 2016-07-26 Array Biopharma Inc piperdinyl-substituted lactams as gpr119 modulators
CN103119045B (en) 2010-08-20 2016-02-17 和记黄埔医药（上海）有限公司 Pyrrolopyrimidine compounds and uses thereof
EP2632898A4 (en) 2010-10-29 2014-04-02 Biogen Idec Inc Heterocyclic tyrosine kinase inhibitors
JP2014517016A (en) * 2011-06-10 2014-07-17 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Pyrimidine having BTK inhibitory activity and composition of pyrimidine compound and method for producing the same
US9029370B2 (en) 2011-06-10 2015-05-12 Hoffmann-La Roche Inc. Substituted benzamide derivatives
CN103732596B (en) * 2011-07-08 2016-06-01 诺华股份有限公司 Pyrrolopyrimidine derivatives
US9138436B2 (en) 2011-07-13 2015-09-22 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
EP2766355B1 (en) 2011-10-11 2020-12-23 Dana-Farber Cancer Institute, Inc. Pyrazol-3-ones that activate pro-apoptotic bax
US9221809B2 (en) 2011-10-31 2015-12-29 Merck Sharp & Dohme Corp. Aminopyrimidinones as interleukin receptor-associated kinase inhibitors
EP2773639B1 (en) * 2011-11-03 2017-04-26 F. Hoffmann-La Roche AG Alkylated piperazine compounds as inhibitors of btk activity
BR112014010391A2 (en) * 2011-11-03 2017-04-18 Hoffmann La Roche compound, pharmaceutical composition, process of producing a pharmaceutical composition, method of treatment, kit and use of a pharmaceutical composition
CN104203937A (en) * 2011-11-03 2014-12-10 霍夫曼-拉罗奇有限公司 8-fluorophthalazin-1 (2h) - one compounds as inhibitors of btk activity
UA111756C2 (en) * 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг HETEROARYLPYRIDONE AND AZAPIRIDONE COMPOUNDS AS BRUTON TYROSINKINASE INHIBITORS
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
ES2672367T3 (en) * 2012-01-09 2018-06-14 X-Chem, Inc. Triptoline derivatives that have kinase inhibitory activity and their uses
EP2838898B1 (en) * 2012-04-20 2017-01-18 Advinus Therapeutics Limited Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
CN102702110A (en) * 2012-05-24 2012-10-03 盛世泰科生物医药技术(苏州)有限公司 Preparation method of 4-amino-5, 6-dichloropyrimidine
US9353087B2 (en) * 2012-06-08 2016-05-31 Biogen Ma Inc. Inhibitors of Bruton's tyrosine kinase
AR091273A1 (en) 2012-06-08 2015-01-21 Biogen Idec Inc PYRIMIDINYL TIROSINE KINASE INHIBITORS
KR20180088926A (en) 2012-07-24 2018-08-07 파마싸이클릭스 엘엘씨 Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
RU2619465C2 (en) * 2012-10-26 2017-05-16 Ф. Хоффманн-Ля Рош Аг Bruton's tyrosine kinase inhibitors
EA201500393A1 (en) * 2012-11-02 2016-05-31 Пфайзер Инк. BLUTON TYROSINKINASE INHIBITORS
CN103848810A (en) * 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 Bruton's tyrosine kinases inhibitor
EP2989106B1 (en) 2013-04-25 2016-12-14 Beigene, Ltd. Fused heterocyclic compounds as protein kinase inhibitors
LT3013337T (en) 2013-06-26 2019-01-10 Abbvie Inc. Primary carboxamides as btk inhibitors
CN112552401B (en) 2013-09-13 2023-08-25 广州百济神州生物制药有限公司 anti-PD 1 antibodies and their use as therapeutic and diagnostic agents
CA2925124A1 (en) 2013-09-30 2015-04-02 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
ES2654051T3 (en) 2013-12-05 2018-02-12 Pfizer Inc. Pyrrolo [2,3-d] pyrimidinyl, pyrrolo [2,3-b] pyrazinyl and pyrrolo [2,3-d] pyridinyl acrylamides
AR098721A1 (en) * 2013-12-11 2016-06-08 Biogen Idec Inc INHIBITORS OF TIROSINA QUINASA DE BRUTON BIARILO
TWI726608B (en) 2014-07-03 2021-05-01 英屬開曼群島商百濟神州有限公司 Anti-pd-l1 antibodies and their use as therapeutics and diagnostics
MA40552A (en) 2014-08-04 2021-05-19 Nuevolution As PYRIMIDINE DERIVATIVES POSSIBLY CONDENSED SUBSTITUTED BY A HETEROCYCLE USEFUL IN THE TREATMENT OF INFLAMMATORY, METABOLIC, ONCOLOGICAL AND AUTOIMMUNE DISEASES
WO2016178110A1 (en) 2015-05-01 2016-11-10 Pfizer Inc. Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, pyrrolo[2,3-b]pyridinyl acrylamides and epoxides thereof
KR102404759B1 (en) * 2016-05-16 2022-05-31 쑤저우 시노벤트 파마슈티칼즈 씨오., 엘티디. 5-Aminopyrazole carboxamide derivatives as BK inhibitors and methods for their preparation and pharmaceutical compositions
JP6993056B2 (en) 2016-07-05 2022-02-15 ベイジーン リミテッド Combination of PD-1 antagonist and RAF inhibitor for cancer treatment
AU2017298035B2 (en) * 2016-07-21 2021-10-28 Biogen Ma Inc. Succinate forms and compositions of Bruton's tyrosine kinase inhibitors
EP4353322A3 (en) 2016-08-16 2024-07-31 BeiGene Switzerland GmbH Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
US11701357B2 (en) 2016-08-19 2023-07-18 Beigene Switzerland Gmbh Treatment of B cell cancers using a combination comprising Btk inhibitors
IL292938A (en) 2016-09-19 2022-07-01 Mei Pharma Inc Combination therapy
MA46995A (en) 2016-12-03 2019-10-09 Acerta Pharma Bv METHODS AND COMPOSITIONS FOR THE USE OF THERAPEUTIC T-LYMPHOCYTES IN COMBINATION WITH KINASE INHIBITORS
TWI774726B (en) 2017-01-25 2022-08-21 英屬開曼群島商百濟神州有限公司 Crystalline forms of (s)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
JOP20190233A1 (en) * 2017-04-14 2019-10-02 Biogen Ma Inc Benzoazepine analogs as inhibiting agents for bruton's tyrosine kinase
AU2018263921A1 (en) 2017-05-03 2019-12-05 Vivace Therapeutics, Inc. Non-fused tricyclic compounds
TW201906866A (en) 2017-06-26 2019-02-16 英屬開曼群島商百濟神州有限公司 Treatment of abnormal bone condition in patients with acid sphingomyelinase deficiency
US11377449B2 (en) 2017-08-12 2022-07-05 Beigene, Ltd. BTK inhibitors with improved dual selectivity
US11192865B2 (en) 2017-08-21 2021-12-07 Vivace Therapeutics, Inc. Benzosulfonyl compounds
CN107445981B (en) * 2017-08-25 2018-06-22 牡丹江医学院 A kind of reactive compound for anti-treating cervicitis
US11786529B2 (en) 2017-11-29 2023-10-17 Beigene Switzerland Gmbh Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors
CA3084648A1 (en) 2017-12-06 2019-06-13 Vivace Therapeutics, Inc. Benzocarbonyl compounds
EP3793551A4 (en) * 2018-05-16 2022-01-26 Vivace Therapeutics, Inc. Oxadiazole compounds
CA3111126A1 (en) 2018-08-31 2020-03-05 Stichting Katholieke Universiteit Synergistic combinations of amino acid depletion agent sensitizers (aadas) and amino acid depletion agents (aada), and therapeutic methods of use thereof
AU2019344107B2 (en) 2018-09-21 2022-09-15 Pfizer Inc. N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamides useful as CCR6 inhibitors
CN109369513B (en) * 2018-11-20 2020-08-25 都创(上海)医药科技有限公司 Preparation method of FBDD common molecular fragment
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220098759A (en) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) A method of treating cancer that has acquired resistance to a kinase inhibitor
MX2022007265A (en) 2019-12-20 2022-09-09 Nuevolution As Compounds active towards nuclear receptors.
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
EP4126875A1 (en) 2020-03-31 2023-02-08 Nuevolution A/S Compounds active towards nuclear receptors
EP4126874A1 (en) 2020-03-31 2023-02-08 Nuevolution A/S Compounds active towards nuclear receptors
WO2022212893A1 (en) 2021-04-02 2022-10-06 Biogen Ma Inc. Combination treatment methods of multiple sclerosis
CN113416847B (en) * 2021-07-05 2022-05-31 昆明理工大学 Method for recycling, reducing and harmlessly treating vanadium extraction tailings
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder
WO2024084360A1 (en) 2022-10-18 2024-04-25 Pfizer Inc. Patatin-like phospholipase domain-containing protein 3 (pnpla3) modifiers
WO2024084363A1 (en) 2022-10-18 2024-04-25 Pfizer Inc. Use of patatin-like phospholipase domain-containing protein 3 compounds

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4528138A (en) 1984-06-20 1985-07-09 E. R. Squibb & Sons, Inc. 16-Keto-17-substituted thia-17-alkyl(or alkenyl or alkynyl) androstenes
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (en) 1985-10-03 1988-12-02 Merck Sharp & Dohme LIQUID-GEL PHASE TRANSITION PHARMACEUTICAL COMPOSITION
JP2594486B2 (en) 1991-01-15 1997-03-26 アルコン ラボラトリーズ インコーポレイテッド Topical ophthalmic composition
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
PA8474101A1 (en) 1998-06-19 2000-09-29 Pfizer Prod Inc PYROLEUM [2,3-D] PIRIMIDINE COMPOUNDS
US6919178B2 (en) * 2000-11-21 2005-07-19 Sunesis Pharmaceuticals, Inc. Extended tethering approach for rapid identification of ligands
CN1481377A (en) 2000-03-17 2004-03-10 ����˹�ж�-����˹˹����ҩƷ��˾ Cyclic Beta-amino acid derivatives as inhibitors of matrix metalloproteases and TNF alhpa
MY145722A (en) 2000-04-27 2012-03-30 Abbott Lab Diazabicyclic central nervous system active agents
DK1686130T3 (en) 2000-06-26 2009-04-06 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine compounds as immunosuppressants
PE20020507A1 (en) 2000-10-17 2002-06-25 Schering Corp NON-IMIDAZOLE COMPOUNDS AS ANTAGONISTS OF THE HISTAMINE H3 RECEPTOR
US20050143372A1 (en) * 2001-10-30 2005-06-30 Shomir Ghosh Compounds, pharmaceutical compositions and methods of use therefor
EP1442039A1 (en) 2001-10-31 2004-08-04 Bayer HealthCare AG Pyrimido (4,5-b) indole derivatives
CN102558155A (en) * 2003-01-14 2012-07-11 阿伦纳药品公司 Aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of diseases related thereto, such as diabetes and hyperglycemia
UA92450C2 (en) * 2003-01-14 2010-11-10 Арена Фармасьютикалз, Инк. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
AU2004282179B2 (en) 2003-10-14 2011-05-19 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein kinase inhibitors
EP1750727A2 (en) 2004-04-23 2007-02-14 Exelixis, Inc. Kinase modulators and methods of use
FR2870541B1 (en) * 2004-05-18 2006-07-14 Proskelia Sas ANTIGONISTIC PYRIMIDINE DERIVATIVES OF VITRONECTIN RECEPTOR
TW200621760A (en) 2004-09-09 2006-07-01 Mitsubishi Pharma Corp 2-morpholino-4-pyrimidone compound
DK1812440T3 (en) 2004-11-04 2011-01-31 Vertex Pharma Pyrazolo [1,5-a] pyrimidines which can be used as inhibitors of protein kinases
EP1819684B1 (en) 2004-12-03 2013-08-07 Intervet International B.V. Substituted piperazines as cb1 antagonists
JP5274842B2 (en) 2004-12-28 2013-08-28 エグゼリクシス， インコーポレイテッド [1H-piperazo [3,4-d] pyrimidin-4-yl] -piperazine as a serine-threonine kinase modulator (p70S6K, Akt-1 and Akt-2) for the treatment of immune, inflammatory and proliferative disorders Or [1H-piperazo [3,4-d] pyrimidin-4-yl] -piperazine compounds
WO2006071875A1 (en) * 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
US7423043B2 (en) * 2005-02-18 2008-09-09 Lexicon Pharmaceuticals, Inc. 4-Piperidin-1-yl-7H-pyrrolo[2,3-d]pyrimidine compounds
US20060281764A1 (en) 2005-06-10 2006-12-14 Gaul Michael D Aminopyrimidines as kinase modulators
US20060281700A1 (en) 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using aminopyrimidines kinase modulators
TW200740779A (en) 2005-07-22 2007-11-01 Mitsubishi Pharma Corp Intermediate compound for synthesizing pharmaceutical agent and production method thereof
EP1951684B1 (en) * 2005-11-01 2016-07-13 TargeGen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
WO2007075555A2 (en) 2005-12-21 2007-07-05 Schering Corporation Combination of an h3 antagonist/inverse agonist and an appetite suppressant
US20080076924A1 (en) 2006-06-30 2008-03-27 Patrick Betschmann Piperazines as P2X7 antagonists
JP2009544732A (en) 2006-07-26 2009-12-17 ノバルティス アクチエンゲゼルシャフト Inhibitors of undecaprenyl pyrophosphate synthase
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
WO2008033858A2 (en) 2006-09-11 2008-03-20 Cgi Pharmaceuticals, Inc. Kinase inhibitors, and methods of using and identifying kinase inhibitors
EP2532235A1 (en) 2006-09-22 2012-12-12 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
CN101674831A (en) 2007-03-02 2010-03-17 先灵公司 Piperidine derivatives and methods of use thereof
WO2008116064A2 (en) 2007-03-21 2008-09-25 Bristol-Myers Squibb Company Fused heterocyclic compounds useful for the treatment of proliferative, allergic, autoimmune or inflammatory diseases
WO2008144253A1 (en) * 2007-05-14 2008-11-27 Irm Llc Protein kinase inhibitors and methods for using thereof
CN101932580B (en) 2007-06-01 2013-05-22 葛兰素史密丝克莱恩有限责任公司 Imidazopyridine kinase inhibitors
AU2009211514B2 (en) 2008-02-05 2014-02-20 F. Hoffmann-La Roche Ag Novel pyridinones and pyridazinones
JP2011519049A (en) 2008-04-29 2011-06-30 イミューンエクサイト インコーポレイテッド Immunomodulatory composition and method of use thereof
CN105362277A (en) 2008-07-16 2016-03-02 药品循环有限公司 Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
BRPI0922565A2 (en) 2008-12-19 2015-12-15 Bristol Myers Squibb Co carbazole carboxamide compounds useful as kinase inhibitors
EP3255047B1 (en) 2009-01-06 2021-06-30 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and uses in treating disorders
JP2012528102A (en) 2009-05-25 2012-11-12 サンド・アクチエンゲゼルシヤフト Method for producing ceftbiprole medcaryl
DK2473049T3 (en) * 2009-09-04 2019-04-01 Biogen Ma Inc INHIBITORS OF BRUTON'S TYROSINKINASE
WO2011029043A1 (en) 2009-09-04 2011-03-10 Biogen Idec Ma Inc. Heteroaryl btk inhibitors
US8685880B2 (en) 2010-06-30 2014-04-01 Chevron U.S.A. Inc. On-site drying of aqueous salt for ionic liquid make-up
EP2632898A4 (en) 2010-10-29 2014-04-02 Biogen Idec Inc Heterocyclic tyrosine kinase inhibitors
US9353087B2 (en) * 2012-06-08 2016-05-31 Biogen Ma Inc. Inhibitors of Bruton's tyrosine kinase
AR091273A1 (en) 2012-06-08 2015-01-21 Biogen Idec Inc PYRIMIDINYL TIROSINE KINASE INHIBITORS
US10280169B2 (en) * 2013-12-11 2019-05-07 Biogen Ma Inc. Biaryl bruton's tyrosine kinase inhibitors
AR098721A1 (en) * 2013-12-11 2016-06-08 Biogen Idec Inc INHIBITORS OF TIROSINA QUINASA DE BRUTON BIARILO
WO2016054627A1 (en) 2014-10-03 2016-04-07 Ohio State Innovation Foundation Biomarkers of bruton tyrosine kinase inhibitor resistance
AU2017298035B2 (en) * 2016-07-21 2021-10-28 Biogen Ma Inc. Succinate forms and compositions of Bruton's tyrosine kinase inhibitors

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